Sign up to receive free email alerts when patent applications with chosen keywords are publishedSIGN UP

Abstract:

An oral composition is provided comprising at least 0.5% by weight of the
composition of pyrophosphate in an orally acceptable carrier, wherein the
pyrophosphate is provided by a mixture of disodium pyrophosphate and
tetrasodium pyrophosphate in a ratio from disodium pyrophosphate to
tetrasodium pyrophosphate in the range of from 1:0.4 to 1:1.2 and wherein
the pH value of the composition is in the range of from 6.0 to 8.0. The
oral composition can be used for prevention and control of tartar and/or
calculus formation.

Claims:

1. A mouthwash oral composition comprising at least 0.5% by weight of the
composition of pyrophosphate in an orally acceptable carrier, wherein the
pyrophosphate is provided by a mixture consisting of disodium
pyrophosphate and tetrasodium pyrophosphate in a ratio from disodium
pyrophosphate to tetrasodium pyrophosphate in the range of from 1:0.4 to
1:1.2, wherein the pH value of the composition is in the range of from
6.0 to 8.0, wherein the orally acceptable carrier comprises less than 11%
alcohol and wherein the maximum level of sodium in the composition is
less than 300 mM.

17. The mouthwash oral composition according to claim 1, wherein the
composition further comprises an acceptance improving agent.

18. The mouthwash oral composition according to claim 1, wherein the
maximum level of sodium in the composition is less than 280 mM.

19. The mouthwash oral composition according to claim 1, wherein the
composition comprises less than 13 mM potassium ions.

20. The mouthwash oral composition according to claim 1, wherein the
composition comprises a crystal prevention score (CPS) in the range of
from 70 to 100.

Description:

TECHNICAL FIELD

[0001] The present invention relates to mouthwash or mouthrinse oral care
compositions, with anti-tartar and anti-calculus effects, wherein said
oral compositions comprise pyrophosphates as active agents. In addition,
said oral compositions are stable against crystal formation in solution
even if the product was frozen and thawed up again.

BACKGROUND OF THE INVENTION

[0002] Oral care products such as dentifrice and mouthwash are routinely
used by consumers as part of their oral care hygiene regimens. It is well
known that oral care products can provide both therapeutic and cosmetic
hygiene benefits to consumers. Therapeutic benefits include caries
prevention which is typically delivered through the use of various
fluoride salts; gingivitis prevention by the use of an antimicrobial
agent such as triclosan, stannous fluoride, or essential oils; or
hypersensitivity control through the use of ingredients such as strontium
chloride or potassium nitrate. Cosmetic benefits provided by oral care
products include the control of plaque and calculus formation, removal
and prevention of tooth stain, tooth whitening, breath freshening, and
overall improvements in mouth feel impression which can be broadly
characterized as mouth feel aesthetics. Calculus and plaque along with
behavioral and environmental factors lead to formation of dental stains,
significantly affecting the aesthetic appearance of teeth. Behavioral and
environmental factors that contribute to teeth staining propensity
include regular use of coffee, tea, cola or tobacco products, and also
the use of certain oral products containing ingredients that promote
staining, such as chlorhexidine and stannous salts.

[0003] While the art has addressed some of the formulation issues of oral
care products relating to cosmetic benefits, there continues to be a need
in stain prevention and anti-calculus formation from products for daily
use such as dentifrice and mouthwash. The tooth structures that are
generally responsible for presenting a stained appearance are enamel,
dentin, and the acquired pellicle. Extrinsic staining of the acquired
pellicle can arise as a result of compounds, such as tannins and other
polyphenolic compounds that have become trapped in and tightly bound to
the proteinaceous layer on the surface of the teeth. Discoloration from
this type of staining can usually be removed by mechanical methods of
tooth cleaning.

[0004] In contrast, intrinsic staining occurs when the staining compounds
penetrate the enamel and even the dentin, or alternatively, such staining
arises from sources within the tooth. Discoloration from intrinsic
staining is not readily amenable to mechanical methods of tooth cleaning.
Chemical methods, which utilize substances that can penetrate into the
tooth structure, are usually required to eliminate such discoloration.
Thus, for oral care products for daily use such as dentifrice and
mouthwash to provide overall cleaning, it is necessary to add ingredients
for provision of antiplaque and anticalculus benefits as well as stain
removal and stain control. Such ingredients for removal and control of
stain and calculus include abrasives for mechanical cleaning and
bleaches, surfactants and chemical chelants for chemical cleaning. Dental
abrasives provide important whitening benefits, particularly on `brushed`
areas of teeth, but unfortunately are of limited effect in controlling
aesthetically undesirable stains that form along the gumline and
interproximally. The stain is mechanically abraded through the use of
abrasives or polishing agents normally employed in toothpaste
preparations. Bleaches such as urea peroxide, hydrogen peroxide or
calcium peroxide, represent the most common forms of whitening agents for
teeth. It is believed that peroxides whiten teeth by releasing hydroxyl
radicals capable of breaking down the plaque/stain complex into a form
that can be flushed away or removed by an abrasive. However, bleaches
added to dentifrice and mouthwash, are typically present in low
concentrations due to stability and safety limits unique to these product
types. At these low concentrations, bleaches which are oxidizing agents
have not generally been effective at tooth whitening and stain control.
Bleaches and abrasives do not functionally act to prevent acquisition of
stains. Abrasive use can reduce rates of stain acquisition by daily
removal of newly acquired stains, but this action is a `treatment` for
existing stain, not a preventive chemical action.

[0005] Chelants have been suggested in the art for the purpose of
retarding calculus formation and removing calculus after it is formed.
The chemical approach to calculus inhibition generally involves chelation
of calcium ion and/or crystal growth inhibition which prevents the
calculus from forming and/or breaks down mature calculus by removing
calcium. In addition, chemical chelants can in principle remove stains by
binding to teeth surfaces thereby displacing color bodies or chromagens
that cause staining. The retention of these chelants can also prevent
stains from accruing due to disruption of binding sites of color bodies
on tooth surfaces. A number of agents with chelating properties for use
in controlling plaque, calculus and stain have been disclosed in the art.
For example, ethylenediaminetetraacetic acid, nitrilotriacetic acid and
related compounds are disclosed in British Patent 490,384, Feb. 15, 1937;
polyphosphonates in U.S. Pat. No. 3,678,154, Jul. 18, 1972 to Widder et
al., U.S. Pat. No. 5,338,537 issued Aug. 16, 1994 to White, Jr., and U.S.
Pat. No. 5,451,401 issued Sep. 19, 1995 to Zerby et al.; carbonyl
diphosphonates in U.S. Pat. No. 3,737,533, Jun. 5, 1973 to Francis; a
zinc-polymer combination formed by the reaction or interaction of a zinc
compound with an anionic polymer containing carboxylic, sulfonic and/or
phosphonic acid radicals in U.S. Pat. No. 4,138,477, issued Feb. 6, 1979,
to Gaffar; tartaric acid in U.S. Pat. Nos. 5,849,271 issued Dec. 15, 1998
and 5,622,689 issued Apr. 22, 1997 both to Lukacovic; acid or salt form
of tartrate monosuccinate, tartrate disuccinate, and mixtures thereof in
U.S. Pat. No. 5,015,467 issued May 14, 1991 to Smitherman; acrylic acid
polymer or copolymer in U.S. Pat. No. 4,847,070, Jul. 11, 1989 to Pyrz et
al. and in U.S. Pat. No. 4,661,341, Apr. 28, 1987 to Benedict et al.;
sodium alginate in U.S. Pat. No. 4,775,525, issued Oct. 4, 1988, to Pera;
polyvinyl pyrrolidone in GB 741,315 published Nov. 30, 1955, WO 99112517
published Mar. 18, 1999 and U.S. Pat. Nos. 5,538,714 issued Jul. 23, 1996
to Pink et al.; and copolymers of vinyl pyrrolidone with carboxylates in
U.S. Pat. Nos. 5,670,138 issued Sep. 23, 1997 to Venema et al. and in JP
Publication No. 2000-0633250 to Lion Corporation, published Feb. 29,
2000.

[0007] However, pyrophosphates are hardly to stabilize regarding both
degradation and crystallization. This problem becomes even higher in
aqueous solutions, such as mouthwashes or mouthrinses. Thus, it is the
object of the present invention to provide an aqueous solution, e.g. in
the form of a mouthwash or mouthrinse, which comprises pyrophosphates for
calculus and stain prevention and which is stable in solution against
crystallization, even if the composition was frozen and thawed up again.

SUMMARY OF THE INVENTION

[0008] Without being bound to a theory it was surprisingly found that
pyrophosphate is stabilized in solution, in particular against
crystallization, by formulating the pyrophosphate as a mixture of
disodium pyrophosphate and tetrasodium pyrophosphate in a special ratio
in a special carrier solution, wherein the taste of the composition
becomes more favorable.

[0009] According to one aspect there is provided a mouthwash or mouthrinse
oral composition comprising at least about 0.5% by weight of the
composition of pyrophosphate in an orally acceptable carrier, wherein the
pyrophosphate is provided by a mixture of disodium pyrophosphate and
tetrasodium pyrophosphate in a ratio from disodium pyrophosphate to
tetrasodium pyrophosphate in the range of from about 1:0.4 to about
1:1.2, wherein the maximum level of sodium in the composition is less
than 300 mM and wherein the pH value of the composition is in the range
of from about 6.0 to about 8.0. The orally acceptable carrier comprises
preferably less than 11% alcohol.

[0010] According to another aspect there is disclosed the cosmetic use of
a mouthwash or mouthrinse oral composition comprising at least about 0.5%
by weight of the composition of pyrophosphate in an orally acceptable
carrier, wherein the pyrophosphate is provided by a mixture of disodium
pyrophosphate and tetrasodium pyrophosphate in a ratio from disodium
pyrophosphate to tetrasodium pyrophosphate in the range of from about
1:0.4 to about 1:1.2, wherein the maximum level of sodium in the
composition is less than 300 mM and wherein the pH value of the
composition is in the range of from about 6.0 to about 8.0 for cosmetic
anti-tartar and/or anti-calculus control. The orally acceptable carrier
used comprises preferably less than 11% alcohol.

[0011] According to another aspect there is provided a method for
preventing and reducing stain and calculus formation by rinsing the oral
cavity, in particular by rinsing the teeth and the mucosa with about 10
ml of a mouthwash or mouthrinse oral composition comprising at least
about 0.5% by weight of the composition of pyrophosphate in an orally
acceptable carrier, wherein the pyrophosphate is provided by a mixture of
disodium pyrophosphate and tetrasodium pyrophosphate in a ratio from
disodium pyrophosphate to tetrasodium pyrophosphate in the range of from
about 1:0.4 to about 1:1.2 wherein the maximum level of sodium in the
composition is less than 300 mM and wherein the pH value of the
composition is in the range of from about 6.0 to about 8.0 at least twice
a day for at least about 60 sec. The orally acceptable carrier used
comprises preferably less than 11% alcohol.

[0012] These and other features, aspects, and advantages of the present
invention will become evident to those skilled in the art from the
detailed description which follows.

DETAILED DESCRIPTION OF THE INVENTION

[0013] While the specification concludes with claims particularly pointing
out and distinctly claiming the invention, it is believed that the
present invention will be better understood from the following
description.

[0014] All percentages and ratios used hereinafter are by weight of total
composition, unless otherwise indicated. All percentages, ratios, and
levels of ingredients referred to herein are based on the actual amount
of the ingredient, and do not comprise solvents, fillers, or other
materials with which the ingredient may be combined as a commercially
available product, unless otherwise indicated.

[0017] As used herein, the word "comprise," and its variants, e.g.
"include", are intended to be non-limiting, such that recitation of items
in a list is not to the exclusion of other like items that may also be
useful in the materials, compositions, devices, and methods of this
invention. This term encompasses the terms "consisting of" and
"consisting essentially of".

[0018] As used herein, the words "preferred", "preferably" and variants
refer to embodiments of the invention that afford certain benefits, under
certain circumstances. However, other embodiments may also be preferred,
under the same or other circumstances. Furthermore, the recitation of one
or more preferred embodiments does not imply that other embodiments are
not useful, and is not intended to exclude other embodiments from the
scope of the invention.

[0019] The compositions herein are useful for topical application, in
particular for topical application in the mouth. I.e. the composition
might be an oral care composition. As used herein, "oral care
composition" is meant a product, which in the ordinary course of usage,
is not intentionally swallowed for purposes of systemic administration of
particular therapeutic agents, but is rather retained in the oral cavity
for a time sufficient to contact substantially all of the dental surfaces
and/or oral tissues for purposes of oral activity. Oral care composition
may be generally in various forms including toothpaste, dentifrice, tooth
gel, subgingival gel, mouthrinse, mouthwash, mouthspray, mousse, foam
lozenge, chewable tablet, chewing gum or denture product. The oral
composition disclosed herein is provided in the form of an aqueous
solution, i.e. the oral composition disclosed herein is provided in the
form of a mouthrinse, a mouthwash or a mouthspray.

[0020] Herein, the terms "tartar" and "calculus" are used interchangeably
and refer to mineralized dental plaque biofilms.

[0021] The term "teeth", as used herein, refers to natural teeth as well
as artificial teeth or dental prosthesis and is construed to comprise one
tooth or multiple teeth.

[0022] Active and other ingredients useful herein may be categorized or
described herein by their cosmetic and/or therapeutic benefit or their
postulated mode of action or function. However, it is to be understood
that the active and other ingredients useful herein can, in some
instances, provide more than one cosmetic and/or therapeutic benefit or
function or operate via more than one mode of action. Therefore,
classifications herein are made for the sake of convenience and are not
intended to limit an ingredient to the particularly stated function(s) or
activities listed. The mouthwashes or rinses as disclosed herein may also
include one or more of actives materials.

[0023] The term "orally acceptable carrier" comprises one or more
compatible solid or liquid excipients or diluents which are suitable for
topical oral administration. By "compatible," as used herein, is meant
that the components of the composition are capable of being commingled
without interaction in a manner which would substantially reduce the
composition's stability and/or efficacy. The carriers or excipients of
the present invention can include the usual and conventional components
of mouthwashes or rinses, as more fully described hereinafter: Mouthwash
or rinse carrier materials typically include, but are not limited to one
or more of water, alcohol, humectants, surfactants, and acceptance
improving agents, such as flavoring, sweetening, coloring and/or cooling
agents. The preferred embodiments of the subject invention are
mouthwashes or rinses comprising for example as carrier material, one or
more of water, ethanol, a humectant, a surfactant, a flavoring agent, a
sweetening agent, a coloring agent and optionally a cooling agent. In
particular the carrier material comprises the mixture of water, ethanol,
a humectant, a surfactant, a flavoring agent, a sweetening agent, and a
coloring agent. Optionally mouthwash or rinse carrier materials comprise
in addition preservatives, buffering agents and mixtures thereof. Typical
mouthwash or rinse carrier materials are for example also disclosed in,
e.g., U.S. Pat. No. 3,988,433 to Benedict. Preparation of such
compositions are well known in the art and their selection will depend on
secondary considerations like taste, cost, and shelf stability, etc..

[0024] The preferred embodiments of the subject invention are mouthwashes
or rinses comprising for example as active materials one or more
anticalculus/anti-tartar agent. In addition, the preferred embodiments of
the subject invention are mouthwashes or rinses comprising for example as
active materials an anticalculus/anti-tartar agent and an anticaries
agent. A suitable anticalculus/anti-tartar agent may be for example a
pyrophosphate source present in a concentration sufficient to provide the
intended effect. A suitable anticaries agent may be for example a
fluoride ion source present in a concentration sufficient to provide the
intended effect.

[0025] Sufficient amounts of fluoride ions to provide anticaries
effectiveness are in the range from about 0.0025% to about 5.0% by
weight, preferably from about 0.005% to about 2.0% by weight of the
composition. A wide variety of fluoride ion-yielding materials can be
employed as sources of soluble fluoride in the present compositions and
methods. Examples of suitable fluoride ion-yielding materials are found
in U.S. Pat. No. 3,535,421 to Briner et al. and U.S. Pat. No. 3,678,154
to Widder et al. Suitable fluoride ion sources comprise, but are not
limited to stannous fluoride, sodium fluoride, potassium fluoride, sodium
monofluorophosphate, indium fluoride, amine fluorides such as Olaflur,
and mixtures thereof. In particular, the fluoride compound used in the
mouthwashes disclosed herein is sodium fluoride or stannous fluoride. If
a sodium free fluoride ion source is chosen, potassium fluoride is
preferred.

[0026] The present compositions comprise a pyrophosphate salt as a source
of pyrophosphate ions to provide the anticalculus and anti-tartar effect.
The pyrophosphate salts useful in the present compositions include the
dialkali metal pyrophosphate salts, tetraalkali metal pyrophosphate
salts, and mixtures thereof, in their unhydrated as well as hydrated
forms. For example disodium dihydrogen pyrophosphate
(Na2H2P2O7) and tetrasodium pyrophosphate
(Na4P2O7), are the preferred species. Pyrophosphate salts
are described in more detail in Kirk-Othmer Encyclopedia of Chemical
Technology, Third Edition, Volume 17, Wiley-Interscience Publishers
(1982).

[0027] In compositions of the present invention, the pyrophosphate salts
are completely dissolved and are stable against crystallization in
solution, even, after the composition was frozen and thawed up again.
Therefore, the pyrophosphate sources are present in the mouthwashes as
disclosed herein in a special ratio. Surprisingly, a special mixture of
dialkali metal and tetraalkali metal pyrophosphates was found to be
particularly stable in solution. The preferred mixture of disodium
pyrophosphate and tetrasodium pyrophosphate being in a ratio from
disodium pyrophosphate to tetrasodium pyrophosphate in the range of about
1:0.4 to about 1:1.2 was found to be stable against crystallization. "To
be stable against crystallization" shall mean herein that the
pyrophosphate is completely soluble and does not build any crystals even
if the solution was frozen and thawed up again. Preferably, the ratio
from disodium pyrophosphate to tetrasodium pyrophosphate is in the range
from about 1:0.5 to about 1:1.1, more preferred in the range from about
1:0.6 to about 1:1.0 and most preferred in the range from about 1:0.7 to
about 1:0.9 in order to further increase the stability against
crystallization.

[0028] The stability against crystallization can be measured as crystal
prevention score (CPS). The CPS corresponds to the time needed until a
composition gets crystal free after being frozen completely. During
thawing the test bottles are secured against any movement or other
mechanical influence. Detailed experimental description is given below in
the experimental section. The CPS used in the present invention is based
on the scoring according to the following table:

[0029] The mouthwash or mouthrinse oral compositions of the present
invention are formulated in order to be stable against crystallizations.
Thus, the compositions of the present invention show high crystal
prevention score (CPS), in particular CPS in the range of from 70 to 100,
preferably from 85 to 100, more preferred from 90 to 100, most preferred
from 95 to 100.

[0030] Free pyrophosphate ions may be present in a variety of protonated
states depending on the pH of the composition. By formulating the
pyrophosphate level in an oral composition the degradation of the
pyrophosphate in solution have to be considered. The final amount of free
pyrophosphate ions in the mouthwash is at least about 0.5% by weight of
the composition. For the intended anticalculus and anti-tartar effect an
amount of free pyrophosphate of at least about 0.5% by weight of the
composition is sufficient for the mouthwashes or mouthrinses as disclosed
herein, wherein the choice of the counter ion does not influence the
anticalculus and anti-tartar efficacy. However, solubilized
pyrophosphates are principally subjected to degradation over time. Thus,
it might be advantageous to formulate higher amounts of pyrophosphates
into the present compositions, for example, the amount of pyrophosphate
may be at least about 1.0% or at least about 1.3% or at least about 1.6%
by weight of the composition depending on the intended storage life time.
Suitable maximal levels of pyrophosphate in the composition are maximal
2.8% by weight of the composition, preferably maximal 2.5% by weight of
the composition, more preferred maximal 2.3% by weight of the
composition. The upper limit of the pyrophosphate in the composition
considers the crystallization potential of the pyrophosphate with
suitable counter-ions as well as the products taste.

[0031] The degradation of the pyrophosphates is for example influenced by
the pH value and the storage temperature of the composition. The lower
the pH value and the higher the storage temperature the higher is the
pyrophosphate degradation. The pH value of the present composition is in
the range from about 6 to about 8, in particular in the range from about
6.5 to about 7.5. Without being bound to a theory it is believed that the
pH value of the present composition does not only influences the
pyrophosphate degradation, but also further stabilizes the pyrophosphates
in solution. The pH value of the mouthwashes or mouthrinses as disclosed
herein can be adjusted by combining the actives and the orally acceptable
carrier in the preferred ranges. If necessary, buffer material can be
added in order to adjust the pH value to the disclosed ranges, but
preferably, the mouthwash compositions as disclosed herein are formulated
without adding buffer agents. In particular, the mouthwash compositions
as disclosed herein do not comprise any acidic pH value adjuster.

[0032] For stabilizing the pyrophosphate ions in solution, in particular
in mouthwash or mouthrinse solution as disclosed herein, the total amount
of sodium has to be considered as well. Sodium pyrophosphate shows a
lower solubility product than the other alkali metal pyrophosphates.
Thus, it is preferred, to control the maximum level of sodium in the
total composition. In particular, the maximum level of sodium in the
composition as disclosed herein should be less than about 300 mM,
preferably less than about 280 mM and more preferred less than about 270
mM. Further, the limitation of the sodium level helps to formulate the
intended pH value without adding further pH-adjuster. Thus, it seems to
be a solution to use other counter ions for the pyrophosphate in the
composition, if higher levels of pyrophosphate are desired. In particular
potassium pyrophosphate is often alternatively used in the prior art.
However, the potassium ion imparts a bitter taste into the composition
which might reduce the consumer acceptance. Thus, in order to impart a
favorable taste it is preferred that the present composition comprises
less than 13 mM of potassium ions. In particular, it is preferred that
the present composition does not comprise any potassium pyrophosphate,
more particular that the present composition does not comprise any
potassium ion.

[0033] In addition, the carrier material of the mouthwash compositions as
disclosed herein is adapted to further stabilize the pyrophosphate ions
in solution. By influencing the dielectric constant of the final solution
the pyrophosphate solubility can be increased by increasing the
dielectric constant. Therefore, carrier compounds that influence the
dielectric constant are chosen accordingly and limited in its amount.

[0034] For example, it is believed that the amount and choice of the
humectant used in the carrier material may further stabilize the
pyrophosphate ions against crystallization in solution. The humectant
serves to give compositions a moist feel to the mouth. Suitable
humectants for use in compositions of the subject invention include
edible polyhydric alcohols such as glycerin, sorbitol, xylitol, butylene
glycol, polyethylene glycol, propylene glycol and trimethyl glycine or
mixture thereof, wherein glycerin, propylene glycol, sorbitol (70%
solution) or a mixture thereof is preferred. In addition, the maximum
amount of the humectant should be limited as high levels of humectants
show crystallization promoting activities. A maximum amount of about 8%
by weight of the composition is preferred for the present compositions
and the minimal amount should not be less than about 4% by weight of the
composition. Thus, the mouthwash compositions as disclosed herein
comprises preferably a humectant in the range of from about 4% to about
8%, more preferred in the range of from about 4.5% to about 7%, more
preferred in the range of from about 5% to about 6% by weight of the
composition.

[0035] In addition or alternatively, it was surprisingly found that
although alcohol reduces the freezing temperature of the solution the
maximum level of alcohol should be restricted in order to stabilize the
pyrophosphates in mouthwash or mouthrinse solutions. In a preferred
embodiment the composition as disclosed herein comprises less than about
11% alcohol, i.e. ethanol, by weight of the composition. More preferred
the amount of ethanol should be below about 9% and most preferred the
amount of ethanol should be in the range of about 8% to about 9% by
weight of the composition. When the level of alcohol is reduced below 8%
by weight of the composition further preservatives should be included
into the composition. Generally, a composition which is free of further
preservatives is preferred. Without being bound to a theory it is
believed that the ethanol is critical for micro efficacy, influences the
stability of the pyrophosphate against crystallization and influences
taste, e.g. the burning sensation, and consumer acceptance of the whole
composition.

[0036] The present compositions may also comprise surfactants, also
commonly referred to as sudsing agents. Suitable surfactants are those
which are reasonably stable and foam throughout a wide pH range. The
surfactant may be anionic, non-ionic, amphoteric, zwitterionic, cationic,
or mixtures thereof.

[0037] Anionic surfactants useful herein include the water-soluble salts
of alkyl sulfates having from 8 to 20 carbon atoms in the alkyl radical
(e.g., sodium alkyl sulfate) and the water-soluble salts of sulfonated
monoglycerides of fatty acids having from 8 to 20 carbon atoms. Sodium
lauryl sulfate (SLS) and sodium coconut monoglyceride sulfonates are
examples of anionic surfactants of this type. Other suitable anionic
surfactants are sarcosinates, such as sodium lauroyl sarcosinate,
taurates, sodium lauryl sulfoacetate, sodium lauroyl isothionate, sodium
laureth carboxylate, and sodium dodecyl benzenesulfonate. Mixtures of
anionic surfactants can also be employed. Many suitable anionic
surfactants are disclosed by Agricola et al., U.S. Pat. No. 3,959,458,
issued May 25, 1976. The composition may typically comprise an anionic
surfactant at a level of from about 0.01% to about 5%, from about 0.01%
to about 2% in some embodiments, and from about 0.01% to about 1% in
other embodiments by weight of the composition. Another suitable
surfactant is one selected from the group consisting of sarcosinate
surfactants, isothionate surfactants and taurate surfactants. Preferred
for use herein are alkali metal or ammonium salts of these surfactants,
such as the sodium and potassium salts of the following: lauroyl
sarcosinate, myristoyl sarcosinate, palmitoyl sarcosinate, stearoyl
sarcosinate and oleoyl sarcosinate.

[0038] Useful cationic surfactants include derivatives of aliphatic
quaternary ammonium compounds having one long alkyl chain containing from
about 8 to 18 carbon atoms such as lauryl trimethylammonium chloride;
cetyl pyridinium chloride; cetyl trimethylammonium bromide;
di-isobutylphenoxyethyl-dimethylbenzylammonium chloride; coconut
alkyl-trimethylammonium nitrite; cetyl pyridinium fluoride; etc.
Preferred compounds are the quaternary ammonium fluorides described in
U.S. Pat. No. 3,535,421, Oct. 20, 1970, to Briner et al., where said
quaternary ammonium fluorides have detergent properties. Certain cationic
surfactants can also act as germicides in the compositions disclosed
herein. Cationic surfactants such as chlorhexidine, although suitable for
use in the current composition, are not preferred due to their capacity
to stain the oral cavity's hard tissues. Persons skilled in the art are
aware of this possibility and should incorporate cationic surfactants
only with this limitation in mind.

[0039] Nonionic surfactants that can be used in the compositions include
compounds produced by the condensation of alkylene oxide groups
(hydrophilic in nature) with an organic hydrophobic compound which may be
aliphatic or alkylaromatic in nature. Examples of suitable nonionic
surfactants include polysorbates, which are derived from PEG-ylated
sorbitan esterified with fatty acids or poloxamers which are difunctional
block-polymers terminating in primary hydroxyl groups with molecular
weights ranging from 1,000 to above 15,000. Poloxamers are e.g. sold
under the tradename of Pluronics and Pluraflo by BASF. The Pluronics are
polyethylene oxide condensates of alkyl phenols, products derived from
the condensation of ethylene oxide with the reaction product of propylene
oxide and ethylene diamine, ethylene oxide condensates of aliphatic
alcohols, long chain tertiary amine oxides, long chain tertiary phosphine
oxides, long chain dialkyl sulfoxides, and mixtures of such materials.
Suitable poloxamers for this invention are Poloxamer 407 and Pluraflo
L4370 which may also function as an emulsifying agent, binder,
stabilizer, and other related functions. The nonionic surfactant may be
present in the compositions from about 0.1% to about 5%, preferably from
about 0.01% to about 2.0% preferably from about 0.01% to about 1.0% by
weight of the total composition.

[0040] Useful zwitterionic synthetic surfactants include derivatives of
aliphatic quaternary ammonium, phosphonium, and sulfonium compounds, in
which the aliphatic radicals can be straight chain or branched, and
wherein one of the aliphatic substituents contains from 8 to 18 carbon
atoms and one contains an anionic water-solubilizing group, e.g. carboxy,
sulfonate, sulfate, phosphate or phosphonate. Suitable betaine
surfactants are disclosed in U.S. Pat. No. 5,180,577 to Polefka et al.,
issued Jan. 19, 1993. Typical alkyl dimethyl betaines include decyl
betaine or 2-(N-decyl-N,N-dimethylammonio) acetate, cocobetaine or
2-(N-coc-N, N-dimethyl ammonio) acetate, myristyl betaine, palmityl
betaine, lauryl betaine, cetyl betaine, cetyl betaine, stearyl betaine,
etc. The amidobetaines are exemplified by cocoamidoethyl betaine,
cocoamidopropyl betaine, lauramidopropyl betaine and the like. The
betaines of choice are preferably the cocoamidopropyl betaine and, more
preferably, the lauramidopropyl betaine. The composition may typically
comprise a zwitterionic surfactant at a level of from about 0.01% to
about 5%, from about 0.01% to about 2% in some embodiments, and from
about 0.01% to about 1% by weight of the composition.

[0041] The present composition further comprises one or more acceptance
improving agents which are formulated into the composition in order to
improve the taste, the optics or any other property of the composition
which improves the acceptance of the composition by the consumer.
Suitable acceptance improving agents are for example sweetening agents,
coloring agents, flavoring agents, optionally cooling agents or a mixture
thereof.

[0042] Sweetening agents which can be used include sucrose, glucose,
saccharin, sucralose, dextrose, levulose, lactose, mannitol, sorbitol,
fructose, maltose, xylitol, saccharin salts, thaumatin, aspartame,
D-tryptophan, dihydrochalcones, acesulfame and cyclamate salts,
especially sodium cyclamate, sucralose and sodium saccharin, and mixtures
thereof. A composition preferably contains from about 0.01% to about 2.0%
by weight of the composition of these agents, more preferred from about
0.01% to about 1% of these agents, more preferred from about 0.01% to
about 0.1%, by weight of the composition of the sweetening agents.

[0043] Flavoring agents may also be added to the compositions. Examples of
suitable flavoring agents as disclosed in U.S. Pat. No. 4,684,517 to
Clipper et al. include menthol, methyl salicylate, cinnamic aldehyde and
clove oil. Generally, plant oils, such as peppermint or spearmint oil are
often used in oral care compositions. Flavoring agents are generally used
in the compositions at levels of from about 0.001% to about 2%,
preferably from about 0.05% to about 1%, more preferred from about 0.1%
to about 0.5% by weight of the composition.

[0044] In addition to sweetening and flavoring agents or as part of the
flavoring agents cooling agents, salivating agents, warming agents, and
numbing agents can be used as optional ingredients in the compositions.
These agents are present in the compositions at a level of from about
0.001% to about 2%, preferably from about 0.01% to about 1%, by weight of
the composition.

[0045] The cooling agent can be any of a wide variety of materials.
Included among such materials are carboxamides, menthol, ketals, diols,
and mixtures thereof. Preferred cooling agents in the present
compositions are the paramenthan carboxyamide agents such as
N-ethyl-p-menthan-3-carboxamide, known commercially as "WS-3",
N,2,3-trimethyl-2-isopropylbutanamide, known commercially as `WS-23,"
Ethyl 3-(p-menthane-3-carboxamido)acetate known commercially as "WS-5",
(1R,2S,5R)-N-(4-Methoxyphenyl)-p-menthanecarboxamide known commercially
as "WS-12", (1R,2S,5R)-N-(4-(cyanomethyl)phenyl)menthylcarboxamide known
commercially as "G-180" and mixtures thereof. Additional preferred
coolants are selected from the group consisting of menthol,
3-1-menthoxypropane-1,2-diol known as TK-10 manufactured by Takasago,
menthone glycerol acetal known as MGA manufactured by Haarmann and
Reimer, and menthyl lactate known as Frescolat® manufactured by
Haarmann and Reimer. The terms menthol and menthyl as used herein include
dextro- and levorotatory isomers of these compounds and racemic mixtures
thereof. TK-10 is described in U.S. Pat. No. 4,459,425, Amano et al.,
issued Jul. 10, 1984. WS-3 and other agents are described in U.S. Pat.
No.4,136,163, Watson, et al., issued Jan. 23, 1979.

[0047] The coloring agents can be any of a wide variety of materials. Any
orally acceptable coloring agent can be used depending on the intended
color. The coloring agent can be added as solid or liquid. Suitable
coloring agents are for example blue or green colors. These agents are
present in the compositions e.g. at a level of from about 0.0001% to
about 0.2%, preferably from about 0.0001% to about 0.1%, more preferred
from about 0.0001% to about 0.01% by weight of the composition.

[0048] The oral compositions as disclosed herein are mouthwash or
mouthrinse compositions. Thus, the compositions are aqueous solutions and
comprise a main amount of water in the carrier. Suitable amounts of water
are for example in the range of from 60% to 95%, preferably from 65% to
90%, more preferred from 70% to 85% by weight of the composition.

[0049] In the following a few example embodiments are given of suitable
carrier(s) for the oral mouthwash compositions as disclosed herein. The
mouthwashes or rinses comprising for example as carrier material from 60%
to 95% of water, less than 12% ethanol, from 4% to 8% of a humectant,
from 0.01% to 5% of a surfactant, from 0.01% to 2% of a flavoring agent,
from 0.01% to 2% of a sweetening agent and from 0.0001% to 0.2% of a
coloring agent by weight of the composition or a mixture of one or more
of these carrier materials. In particular, the carrier materials of the
mouthwashes or rinses as disclosed herein may comprise for example a
mixture of from 65% to 90% of water, less than 11% ethanol, from 4.5% to
7% of a humectant, from 0.01% to 2% of a surfactant, from 0.05% to 1% of
a flavoring agent, from 0.01% to 1% of a sweetening agent and from
0.0001% to 0.1% of a coloring agent by weight of the composition or a
mixture of one or more of these carrier materials. Further preferred
suitable carrier materials for the mouthwashes or rinses as disclosed
herein may comprise a mixture of from 70% to 85% of water, from 8% to 9%
ethanol, from 5% to 6% of a humectant, from 0.01% to 1% of a surfactant,
from 0.1% to 0.5% of a flavoring agent, from 0.01% to 0.1% of a
sweetening agent and from 0.0001% to 0.01% of a coloring agent by weight
of the composition.

[0050] These example carrier mixtures may be for example combined with
active materials providing e.g. anticalculus/anti-tartar effects, such as
a mixture of disodium pyrophosphate and tetrasodium pyrophosphate in a
ratio from disodium pyrophosphate to tetrasodium pyrophosphate in the
range of about 1:0.4 to about 1:1.2, wherein the composition comprises a
pH in the range of from about 6.0 to about 8.0. In particular, the
example carrier mixtures may be combined with active materials such as a
mixture of disodium pyrophosphate and tetrasodium pyrophosphate in a
ratio from disodium pyrophosphate to tetrasodium pyrophosphate in the
range of from about 1:0.7 to about 1:0.9, wherein the composition
comprises a pH in the range of from about 6.5 to about 7.5.

[0051] If anticaries benefits shall be provided in addition, an anticaries
agent can be combined with the anticalculus agents. Thus, these example
carrier mixtures may be for example combined with active materials such
as at least about 0.0025% by weight of the composition of fluoride ions
and a mixture of disodium pyrophosphate and tetrasodium pyrophosphate in
a ratio from disodium pyrophosphate to tetrasodium pyrophosphate in the
range of about 1:0.4 to about 1:1.2, wherein the composition comprises a
pH in the range of from about 6.0 to about 8.0. In particular, the
example carrier mixtures may be combined with active materials such as at
least about 0.005% by weight of the composition of fluoride ions and a
mixture of disodium pyrophosphate and tetrasodium pyrophosphate in a
ratio from disodium pyrophosphate to tetrasodium pyrophosphate in the
range of from about 1:0.7 to about 1:0.9, wherein the composition
comprises a pH in the range of from about 6.5 to about 7.5.

[0052] As the present composition provides anti-tartar and/or
anti-calculus control benefits the disclosed compositions can be used for
anti-tartar and/or anti-calculus control. For controlling tartar and
preventing staining of the teeth a subject's dental enamel surfaces and
mucosa in the mouth should be contacted with the oral compositions
according to the present invention. Contacting may be rinsing with a
mouthwash or mouthrinse. The subject may be any person or animal whose
tooth surface contacts the oral composition. By animal is meant to
include household pets or other domestic animals, or animals kept in
captivity. Example would include the rinsing of a cat's mouth with an
oral composition for a sufficient amount of time to see a benefit. A
benefit can be for example seen by rinsing the dental enamel surfaces and
mucosa twice a day for at least 30 sec with the 20 ml of the composition
as disclosed herein alternatively by rinsing the dental enamel surfaces
and mucosa twice a day for at least 60 sec with 10 ml product.

EXAMPLES

[0053] The following examples further describe and demonstrate embodiments
within the scope of the present invention. These examples are given
solely for the purpose of illustration and are not to be construed as
limitations of the present invention as many variations thereof are
possible without departing from the spirit and scope.

Example I

Crystal Prevention Score (CPS)

[0054] The stability against crystallization can be measured as crystal
prevention score (CPS). The CPS corresponds to the time needed until a
composition gets crystal free after being frozen completely. For
determining the CPS the composition in multiple 500 ml clear bottles (3-6
bottles per composition) to be tested is frozen at lower than -18°
C. for at least 24h. Then these bottles are transferred to room
temperature or to a 2-5° C. refrigerator and the time until all
bottles get crystal free is measured. During thawing these bottles are
secured against any movement or other mechanical influence. Some of the
experiments are repeated 2-3 times. Results will be averaged, if not all
bottles of the same composition get crystal free at the same time.
Therefore, the results are averaged and the CPS is determined according
to the following table:

[0055] Mouthwash compositions according to the present invention (Examples
IA-IH) are shown below with amounts of components in % by weight of the
composition. These compositions are made using conventional methods, in
particular as given in Example III. The CPS for each composition was
measured and is given below.

[0056] One suitable method is given to manufacture the compositions as
disclosed herein. Deviations of said method and alternatives are possible
and can be considered by the skilled person. The dye is solved in a part
of the water in order to form a dye premix. For solving the dye
completely the dye premix is agitated for at least 10 min without
splashing. In parallel a flavor premix is produced by adding the flavors
into the ethanol under continuous agitation without splashing. Then a
part of the surfactant is added to the flavor premix and the flavor
premix is agitated for at least 10 min. Then the remaining water is added
in a main mix tank where water temperature is maintained between 20 to
30° C. Under continuous agitation without splashing first the
tetrasodium pyrophosphate followed by the disodium pyrophosphate is added
slowly in order to avoid clumping. After at least 5 min of agitation, the
rest of the surfactant, sweeteners and sodium fluoride are added under
moderate agitation so that excessive foam formation is avoided. Then the
agitation speed is further reduced and the glycerin is added to the main
mix followed by the dye premix and the flavor premix. The final
composition is then mixed for at least 20 min until a homogeneous
composition is received.

Example IV

Consumer Acceptance

[0057] Example IB was tested against the comparative Example which is a
product currently on the market regarding the overall performance and
consumer acceptance by 12 people who were willing to use a mouthwash.
Blind paired comparison tests were performed at three days. In each
category people were asked to give their rate of agreement with the
questions asked.

[0060] Example IB was found by the consumer to be less bitter, induces
less burning and received a better overall acceptance with having a
better taste. The overall rate is nearly 2 times better versus the
Comparative Example.

[0061] In a second test trained sensory panelists compared Example IB and
the Comparative

[0063] The trained panelists confirmed that the composition as disclosed
herein imparts less burning sensation in the mouth as well as over time.
Bitterness of the composition of Example IB was considered less directly
after expectoration. The in mouth value is comparable to the bitterness
of the Comparative Example.

[0064] That means, in addition to be stabilized against crystal formation
in solution the compositions as disclosed herein show also taste
advantages and a better Consumer acceptance compared to the marketed
Comparative Example.

[0065] The dimensions and values disclosed herein are not to be understood
as being strictly limited to the exact numerical values recited. Instead,
unless otherwise specified, each such dimension is intended to mean both
the recited value and a functionally equivalent range surrounding that
value. For example, a dimension disclosed as "40 mm" is intended to mean
"about 40 mm."

[0066] All documents cited in the Detailed Description of the Invention
are, in relevant part, incorporated herein by reference; the citation of
any document is not to be construed as an admission that it is prior art
with respect to the present invention.

[0067] While particular embodiments of the present invention have been
illustrated and described, it would be obvious to those skilled in the
art that various other changes and modifications can be made without
departing from the spirit and scope of the invention. It is therefore
intended to cover in the appended claims all such changes and
modifications that are within the scope of this invention.

Patent applications by William Michael Glandorf, Mason, OH US

Patent applications in class Fluorine or fluorine compound containing

Patent applications in all subclasses Fluorine or fluorine compound containing